Affiliations 

  • 1 Faculty of Pharmacy, AIMST University, Semeling, 08100 Bedong, Kedah, Malaysia. Electronic address: hriday.bera1@gmail.com
  • 2 Faculty of Pharmacy, AIMST University, Semeling, 08100 Bedong, Kedah, Malaysia
  • 3 Department of Pharmaceutical Science, Dibrugarh University, Dibrugarh 786004, Assam, India
  • 4 Department of Pharmaceutical Technology, Jadavpur University, Kolkata, West Bengal 700032, India
Int J Biol Macromol, 2019 May 15;129:552-563.
PMID: 30707999 DOI: 10.1016/j.ijbiomac.2019.01.171

Abstract

Novel diethanolamine-grafted high-methoxyl pectin (DGP)-arabic gum (AG) modified montmorillonite (MMT) composites were developed for intragastric ziprasidone HCl (ZIP) delivery by combining floating and mucoadhesion mechanisms. The ZIP-loaded clay-biopolymer matrices were accomplished by ionotropic gelation protocol utilizing zinc acetate in the presence or absence of covalent crosslinker, glutaraldehyde (GA). Various formulations exhibited excellent drug entrapment efficiency (DEE, %) and sustained drug release profiles, which were influenced by the polymer-blend (DGP:AG) ratios, reinforcing filler (MMT) existence and crosslinking procedure. The optimal composites (F-3) demonstrated DEE of 61% and Q8h of 52% with outstanding buoyancy, mucin adsorption ability and biodegradability. The release profile of F-3 was best fitted in the Korsmeyer-Peppas model with Fickian diffusion driven mechanism. The mucin adsorption to composites F-3 followed Freundlich isotherms. The molar mass between crosslinks of composites (F-3) calculated employing Flory-Rehner equation was increased with temperature. Moreover, the thermal, X-ray and infrared analyses confirmed a compatible environment of drug in the composites, except certain extent of transformation of the crystalline drug to its amorphous form. The SEM studies revealed the spherical morphology of the composites. Thus, the newly developed DGP-AG-MMT composites are appropriate for gastroretentive ZIP delivery over an extended period of time.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.